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来源于海洋来源的坦扎瓦酸衍生物作为 RANKL 诱导的破骨细胞生成的抑制剂。

Tanzawaic Acid Derivatives from the Marine-Derived as Inhibitors of RANKL-Induced Osteoclastogenesis.

机构信息

CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, People's Republic of China.

University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing 100049, People's Republic of China.

出版信息

J Nat Prod. 2023 May 26;86(5):1171-1178. doi: 10.1021/acs.jnatprod.2c00865. Epub 2023 Feb 1.

Abstract

Seven new tanzawaic acid derivatives, steckwaic acids E-K (-), and one new benzene derivate (), together with seven known tanzawaic acid analogues (-) were isolated from the marine algicolous fungus SCSIO 41040. The structures and absolute configurations of these new compounds (-) were determined by spectroscopic analyses, X-ray diffraction, and comparison of ECD spectra to calculations. Compounds , , and inhibited lipopolysaccharide (LPS)-induced nuclear factor kappa-B (NF-κB) with IC values of 10.4, 18.6, and 15.2 μM, respectively. Compound could suppress the receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation in bone marrow macrophage cells (BMMCs). To the best of our knowledge, this is the first report of osteoclastogenesis inhibitory activity for tanzawaic acid derivatives.

摘要

从海洋藻类真菌 SCSIO 41040 中分离得到了 7 种新的坦扎瓦酸衍生物(Steckwaic 酸 E-K(-))和 1 种新的苯衍生物(),以及 7 种已知的坦扎瓦酸类似物(-)。通过光谱分析、X 射线衍射和与计算的 ECD 光谱比较,确定了这些新化合物(-)的结构和绝对构型。化合物、和抑制脂多糖(LPS)诱导的核因子 kappa-B(NF-κB),IC 值分别为 10.4、18.6 和 15.2 μM。化合物可以抑制核因子 kappa-B 配体(RANKL)诱导的破骨细胞分化在骨髓巨噬细胞(BMMCs)中。据我们所知,这是坦扎瓦酸衍生物具有破骨细胞生成抑制活性的首次报道。

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